PBRM1-BD2-IN-2

CAS No. 2819989-57-4

PBRM1-BD2-IN-2( —— )

Catalog No. M35349 CAS No. 2819989-57-4

PBRM1-BD2-IN-2, a selective and cell-active inhibitor of the polybromo-1 (PBRM1) bromodomain, exhibits binding affinity and inhibitory activity specifically targeting the PBRM1-BD2 domain, with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
1 mL x 10 mM in DMSO 245 In Stock
5MG 255 In Stock
10MG 375 In Stock
25MG 562 In Stock
50MG 770 In Stock
100MG 1051 In Stock
200MG Get Quote In Stock
500MG 2111 In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    PBRM1-BD2-IN-2
  • Note
    Research use only, not for human use.
  • Brief Description
    PBRM1-BD2-IN-2, a selective and cell-active inhibitor of the polybromo-1 (PBRM1) bromodomain, exhibits binding affinity and inhibitory activity specifically targeting the PBRM1-BD2 domain, with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively.
  • Description
    PBRM1-BD2-IN-2 is a selective and cell-activepolybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-2 has binding affinity and inhibitory activity for PBRM1-BD2 with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. PBRM1-BD2-IN-2 can be used for the research of cancer.
  • In Vitro
    PBRM1-BD2-IN-2 (0, 0.1, 1, and 10 μM; 5 days) selectively inhibit growth of a PBRM1-dependent prostate cancer cell line.PBRM1-BD2-IN-2 has binding affinity for PBRM1-BD2, PBRM1-BD5, SMARCA2B amd SMARCA4 with Kd values of 9.3 μM, 10.1 μM, 18.4 μM and 69 μM, respectively.PBRM1-BD2-IN-2 has inhibitory activity for PBRM1-BD2 with IC50 value of 1.0 μM.Cell Viability Assay Cell Line:Human prostate cell lines LNCaP, PC3, and RWPE-1Concentration:0, 0.1, 1, and 10 μM Incubation Time:5 days Result:Inhibited LNCaP growth at higher concentrations.
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Chromatin/Epigenetic
  • Target
    Epigenetic Reader Domain
  • Recptor
    Epigenetic Reader Domain
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2819989-57-4
  • Formula Weight
    311.14
  • Molecular Formula
    C14H9Cl2FN2O
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    O=C1C=2C(NC(N1)C3=C(Cl)C=CC=C3F)=CC=CC2Cl
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Shifali Shishodia, et al. Selective and Cell-Active PBRM1 Bromodomain Inhibitors Discovered through NMR Fragment Screening. J Med Chem. 2022 Oct 13.?
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